SR141716A, a potent and selective antagonist of the brain cannabinoid receptor

FEBS Letters

Calandra, Bernard³  Maruani, Jeanne²  Martinez, Serge²  Ferrara, Pascual³  Barth, Francis²  Caput, Daniel³  Le Fur, Gérard²  Brelière, Jean Claude²  Shire, David³  Héaulme, Michel²  Congy, Christian²  Soubrié, Philippe²  Néliat, Gervais¹  Rinaldi-Carmona, Murielle² 

[1] Cerep, Le Bois l'Evêque, 86600 Celle l'Evescault, France;Sanofi Recherche, 371 rue du Professeur Blayac, 34184 Montpellier Cedex 04, France;Sanofi Recherches, 31676 Labège, France

关键词: Cannabinoid receptor;    Receptor antagonist;    cAMP;    Behavioural responses;    Tris;    Tris-[hydroxymethyl]aminomethane;    Δ9-THC;    tetrahydrocannabinol;    i.p.;    intraperitoneal;    p.o.;    per os;    i.v.;    intravenous;    CHO;    chinese hamster ovary;   

DOI  :  10.1016/0014-5793(94)00773-X

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

SR141716A is the first selective and orally active antagonist of the brain cannabinoid receptor. This compound displays nanomolar affinity for the central cannabinoid receptor but is not active on the peripheral cannabinoid receptor. In vitro, SR141716A antagonises the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and adenylyl cyclase activity in rat brain membranes. After intraperitoneal or oral administration SR141716A antagonises classical pharmacological and behavioural effects of cannabinoid receptor agonists. This compound should prove to be a powerful tool for investigating the in vivo functions of the anandamide/cannabinoid system.

【 授权许可】

Unknown